US4340730AExpiredUtility

N6 -Substituted adenosines

Assignee: SEARLE & COPriority: Jun 9, 1980Filed: Jan 30, 1981Granted: Jul 20, 1982

Est. expiryJun 9, 2000(expired)· nominal 20-yr term from priority

Inventors:Richard E. Henderson Nancy J. Malek Alan E. Moormann Barnett S. Pitzele

C07H 19/16

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Claims

Abstract

Novel N 6 -adenosines according to formula I are disclosed. These novel compounds are useful as antihypertensive agents.

Claims

exact text as granted — not AI-modified

We claim: 
     
       1. A compound according to the formula: where in R 1  is:   (a) hydrogen; or   (b) alkyl of from 1 to 6 carbon atoms inclusive; where R 2  is:     (a) 4-(N,N-dimethylaminophenethyl);   (b) --(CH 2 ) n  COOR 5  ; wherein n is an integer from 3 to 11 inclusive;   wherein R 5  is:   (a) hydrogen; or   (b) alkyl of from 1 to 20 carbon atoms, inclusive with the provision that when R 1  is hydrogen and n is 5, R 5  cannot be hydrogen;   (c) 3(11,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl; or wherein R 1  and R 2  taken together with N form a piperazine ring of the formula: ##STR2## wherein R 4  is: (a) ethoxycarbonyl.       
     
     
       2. A compound according to claim 1 wherein R 1  is hydrogen. 
     
     
       3. N 6  -[4-(N,N-dimethylamino)phenethyl]adenosine a compound according to claim 2. 
     
     
       4. A compound according to claim 2 wherein R 2  is --(CH 2 ) n  COOR 5  and R 5  is alkyl of from 1 to 20 carbon atoms inclusive. 
     
     
       5. N 6  -[4-ethoxycarbonyl)butyl]adenosine a compound according to claim 4. 
     
     
       6. A compound according to claim 2 wherein R 2  is --(CH 2 ) n  COOR 5  and R 5  is hydrogen, with the provision that when n is not equal to 5, then R 1  is not Hydrogen. 
     
     
       7. N 6  -(4-carboxybutyl)adenosine a compound according to claim 6. 
     
     
       8. A compound according to claim 1 wherein R 1  is alkyl of from 1 to 6 carbon atoms inclusive. 
     
     
       9. A compound according to claim 8 wherein R 1  is methyl. 
     
     
       10. N 6  -[3-(10,11-dihydro-5H-dibenz[b,f]azepin-5-yl)propyl]-N 6  -methyladenosine a compound according to claim 9. 
     
     
       11. A compound according to claim 8 wherein R 2  is --(CH 2 ) n  COOR 5  and R 5  is hydrogen. 
     
     
       12. N 6  -methyl-N 6  -(3-carboxypropyl)adenosine a compound according to claim 11. 
     
     
       13. A compound according to claim 8 wherein R 2  is --(CH 2 ) n  COOR 5  and R 5  is alkyl of 1 to 20 carbon atoms inclusive. 
     
     
       14. N 6  -methyl-N 6  -[3-ethoxycarbonyl)propyl]adenosine a compound according to claim 13. 
     
     
       15. A compound according to claim 1 wherein R 1  and R 2  taken together with N form a piperazine ring of formula II. 
     
     
       16. 6-[4-ethoxycarbonyl)-1-piperazinyl]purine riboside, a compound according to claim 15.

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